The discovery of equipotent PPARalpha/gamma dual activators.
We report the design and synthesis of equipotent PPARalpha/gamma dual agonists starting from selective PPAR alpha agonist 1. In vivo data for 7 in the Zucker fa/fa rat are presented.
Martres
Paul
P
Department of Medicinal Chemistry, Laboratoire GlaxoSmithKline, Centre de Recherches, 25-27 avenue du Québec, 91951 Les Ulis, France. paul.martres@gsk.com
Faucher
Nicolas
N
Laroze
Alain
A
Pineau
Olivier
O
Fouchet
Marie Helene
MH
Potvain
Florent
F
Grillot
Didier
D
Beneton
Veronique
V
D000818:Animals; D020650:Combinatorial Chemistry Techniques; D015195:Drug Design; D015394:Molecular Structure; D047493:PPAR alpha / Q000819:agonists*; D047495:PPAR gamma / Q000819:agonists*; D020033:Protein Isoforms; D011720:Pyrazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000633:toxicity; D051381:Rats; D011924:Rats, Zucker; D013329:Structure-Activity Relationship
D047493:PPAR alpha; D047495:PPAR gamma; D020033:Protein Isoforms; D011720:Pyrazoles